FAK Inhibitor 14

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Cat.No. 3414 - FAK Inhibitor 14 | C6H10N4.4HCl | CAS No. 4506-66-5
Description: Selective FAK inhibitor
Alternative Names: Y15, NSC 677249
Chemical Name: 1,2,4,5-Benzenetetramine tetrahydrochloride
Datasheet
Citations (16)
Reviews
Literature

Biological Activity

Selective focal adhesion kinase (FAK) inhibitor that displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI. Prevents FAK autophosphorylation at Y397 (IC50 = 1 μM), promotes cell detachment and inhibits cell adhesion in vitro. Exhibits antiproliferative activity in a variety of human tumor cell lines in vitro and in breast cancer cells in vivo.

Technical Data

M. Wt 284.01
Formula C6H10N4.4HCl
Storage Desiccate at RT
CAS Number 4506-66-5
PubChem ID 78260
InChI Key BZDGCIJWPWHAOF-UHFFFAOYSA-N
Smiles NC1=C(N)C=C(N)C(N)=C1.Cl.Cl.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 21.3 75
water 14.2 50

Preparing Stock Solutions

The following data is based on the product molecular weight 284.01. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.75 mM 4.69 mL 23.47 mL 46.95 mL
3.75 mM 0.94 mL 4.69 mL 9.39 mL
7.5 mM 0.47 mL 2.35 mL 4.69 mL
37.5 mM 0.09 mL 0.47 mL 0.94 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Golubovskaya et al (2008) A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the Y397 site of focal adhesion kinase decreases tumour growth. J.Med.Chem. 51 7405 PMID: 18989950

Hochwald et al (2009) A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle 8 2435 PMID: 19571674


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View Related Products by Product Action

View all Focal Adhesion Kinase Inhibitors

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16 Citations for FAK Inhibitor 14

Citations are publications that use Tocris products. Selected citations for FAK Inhibitor 14 include:

Gutiérrez et al (2015) RECK-Mediated β1-Integrin Regulation by TGF-β1 Is Critical for Wound Contraction in Mice. J Neurosci 10 e0135005 PMID: 26247610

Rengarajan et al (2016) Endothelial Cells Use a Formin-Dependent Phagocytosis-Like Process to Internalize the Bacterium Listeria monocytogenes. PLoS One 12 e1005603 PMID: 27152864

Visavadiya (2016) Integrin-FAK signaling rapidly and potently promotes mitochondrial function through STAT3. Cell Communication and Signaling 14 32 PMID: 27978828

Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749 PMID: 20071540

An et al (2016) Netrin-1 suppresses the MEK/ERK pathway and ITGB4 in pancreatic cancer. Oncotarget 7 24719 PMID: 27034160

Tsai et al (2013) Estradiol and tamoxifen induce cell migration through GPR30 and activation of focal adhesion kinase (FAK) in endometrial cancers with low or without nuclear estrogen receptor α (ERα). PLoS One 8 e72999 PMID: 24039841

Thakur et al (2015) Inhibition of STAT3, FAK and Src mediated signaling reduces cancer stem cell load, tumorigenic potential and metastasis in breast cancer. Sci Rep 5 10194 PMID: 25973915

McLane and Ligon (2015) Palladin mediates stiffness-induced fibroblast activation in the tumor microenvironment. Biophys J 109 249 PMID: 26200861

Barbelanne et al (2013) Pathogenic NPHP5 mutations impair protein interaction with Cep290, a prerequisite for ciliogenesis. Hum Mol Genet 22 2482 PMID: 23446637

Mendoza-Naranjo et al (2013) ERBB4 confers metastatic capacity in Ewing sarcoma. EMBO Mol Med 5 1019 PMID: 23681745

Malenczyk et al (2013) CB1 cannabinoid receptors couple to focal adhesion kinase to control insulin release. J Biol Chem 288 32685 PMID: 24089517

Keasey et al (2013) Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression. Cell Commun Signal 11 35 PMID: 23693126

Wiel et al (2013) Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis. Cell Death Dis 4 e855 PMID: 24113189

Afrikanova et al (2011) Inhibitors of Src and focal adhesion kinase promote endocrine specification: impact on the derivation of β-cells from human pluripotent stem cells. J Biol Chem 286 36042 PMID: 21852242

Webber et al (2015) Combination of heat shock protein 90 and focal adhesion kinase inhibitors synergistically inhibits the growth of non-small cell lung cancer cells. Oncoscience 2 765 PMID: 26501082

Shih et al (2014) Astroglial-derived periostin promotes axonal regeneration after spinal cord injury. Auton Neurosci 34 2438 PMID: 24523534


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